Effects of the Ca2+-antagonists nifedipine, verapamil, flunarizine and of the calmodulin antagonist trifluoperazine on muscarinic cholinergic receptors in rat cerebral cortex

Popova, J.; Staneva-Stoytcheva, D; Mutafova, V.

doi:10.1016/0306-3623(90)90830-f

Cited by 11 publications

(6 citation statements)

References 17 publications

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“…These are unlikely to be involved, however, because their blockage should have caused hyperpolarization, not the observed depolarization of the membrane potential. (2) Muscarinic receptors [34,35]. Their blockage by verapamil would be consistent with the hyperpolarizing action of acetylcholine seen in our experiments, although it would have required substantial tonic release of acetylcholine in the isolated tissue used here.…”

Section: Ionic Characteristics Of the Resting Membrane Potentialsupporting

confidence: 73%

Ionic and pharmacologic characteristics of epithelial cells in a semi‐intact preparation of the rat ventral prostate gland

Mycielska¹,

Szatkowski²,

Djamgoz³

2002

The Prostate

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Section: Ionic Characteristics Of the Resting Membrane Potentialsupporting

confidence: 73%

Ionic and pharmacologic characteristics of epithelial cells in a semi‐intact preparation of the rat ventral prostate gland

Mycielska¹,

Szatkowski²,

Djamgoz³

2002

The Prostate

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“…Through its antioxidant potential, it plays a role in blocking membrane lipid bilayer peroxidation [ 160 ]. Finally, flunarizine also modulates cholinergic transmission by promoting acetylcholine (Ach) release and by altering the expression/affinity of muscarinic receptors [ 161 , 162 ].…”

Section: Migraine Drugs Neurodegenerative Pathways and Cognition: Pro...mentioning

confidence: 99%

Migraine Pharmacological Treatment and Cognitive Impairment: Risks and Benefits

Russo

Rosa

Consoli

et al. 2022

IJMS

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Migraine is a common neurological disorder impairing the quality of life of patients. The condition requires, as an acute or prophylactic line of intervention, the frequent use of drugs acting on the central nervous system (CNS). The long-term impact of these medications on cognition and neurodegeneration has never been consistently assessed. The paper reviews pharmacological migraine treatments and discusses their biological and clinical effects on the CNS. The different anti-migraine drugs show distinct profiles concerning neurodegeneration and the risk of cognitive deficits. These features should be carefully evaluated when prescribing a pharmacological treatment as many migraineurs are of scholar or working age and their performances may be affected by drug misuse. Thus, a reconsideration of therapy guidelines is warranted. Furthermore, since conflicting results have emerged in the relationship between migraine and dementia, future studies must consider present and past pharmacological regimens as potential confounding factors.

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“…Besides its general action as inhibitor of the transmembrane influx of extracellular calcium ions, verapamil, in several brain regions (e.g. cerebral cortex, hippocampus, hypothalamus), acts as an antagonist of muscarinic (Baumgold, 1986;Popova et al, 1990), aand b-adrenergic (Galzin and Langer, 1983;Staneva-Stoytcheva et al, 1990;Staneva-Stoytcheva et al, 1992), dopaminergic (Sitges and Guarneros, 1998), serotoninergic (Taylor and Defeudis, 1984;Adachi and Shoji, 1986;Green et al, 1990;Popova et al, 1991;Shad and Saeed, 2007), and GABAergic receptors (Staneva-Stoytcheva et al, 1991). Thus, it is likely from these findings and the impairments of cholinergic (Hampel et al, 2018), GABAergic (Li et al, 2016), and monoaminergic transmission (Sǐmićet al, 2017) in AD disease that verapamil could modify the neurotransmission in AD.…”

Section: Particularities Of Mechanism Of Action Of Verapamil: Pros and Consmentioning

confidence: 99%

Verapamil and Alzheimer’s Disease: Past, Present, and Future

et al. 2020

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Verapamil is a phenylalkylamine class calcium channel blocker that for half a century has been used for the treatment of cardiovascular diseases. Nowadays, verapamil is also considered as a drug option for the treatment of several neurological and psychiatric disorders, such as cluster headache, bipolar disorders, epilepsy, and neurodegenerative diseases. Here, we review insights into the potential preventive and therapeutic role of verapamil on Alzheimer's disease (AD) based on limited experimental and clinical data. Pharmacological studies have shown that verapamil has a wide therapeutic spectrum, including antihypertensive, anti-inflammatory, and antioxidative effects, regulation of the blood-brain barrier function, due to its effect on P-glycoprotein, as well as adjustment of cellular calcium homeostasis, which may result in the delay of AD onset or ameliorate the symptoms of patients. However, the majority of the AD individuals are on polypharmacotherapy, and the interactions between verapamil and other drugs need to be considered. Therefore, for an appropriate and successful AD treatment, a personalized approach is more than necessary. A well-known narrow pharmacological window of verapamil efficacy may hinder this approach. It is therefore important to note that the verapamil efficacy may be conditioned by different factors. The onset, grade, and brain distribution of AD pathological hallmarks, the time-sequential appearances of AD-related cognitive and behavioral dysfunction, the chronobiologic and gender impact on calcium homeostasis and AD pathogenesis may somehow be influencing that success. In the future, such insights will be crucial for testing the validity of verapamil treatment on animal models of AD and clinical approaches.

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Effects of the Ca2+-antagonists nifedipine, verapamil, flunarizine and of the calmodulin antagonist trifluoperazine on muscarinic cholinergic receptors in rat cerebral cortex

Cited by 11 publications

References 17 publications

Ionic and pharmacologic characteristics of epithelial cells in a semi‐intact preparation of the rat ventral prostate gland

Ionic and pharmacologic characteristics of epithelial cells in a semi‐intact preparation of the rat ventral prostate gland

Migraine Pharmacological Treatment and Cognitive Impairment: Risks and Benefits

Verapamil and Alzheimer’s Disease: Past, Present, and Future

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